pharmacological aspects of calotropis gigantea on various health ...

Anurag Agrawal., et al. / International Journal <strong>of</strong> Advances in Pharmaceutical Research
IJAPR
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Review Article
ISSN: 2230 – 7583
PHARMACOLOGICAL ASPECTS OF CALOTROPIS GIGANTEA ON VARIOUS
HEALTH PROBLEMS: A REVIEW
Anurag Agrawal 1* , Namrata Singh 2 , Pushpendra Kannojia 3 , Virendra Kumar Garg 4
1 R.C.Patel Institute <strong>of</strong> Pharmaceutical Education & Research, Near Karwand Naka, Shirpur Dhule -425405 (M.S.)
2 Department <strong>of</strong> Pharmacy, Barkatullah University, Hoshangabad road, Bhopal- 462026 (M.P.)
3
IPS-College <strong>of</strong> Pharmacy, Bela Ki Bawadi Tiraha, Shivpuri Link Road Gwalior-474001(M.P.)
4
Gurukul Institute <strong>of</strong> Pharmaceutical Sciences & Research, Tighra Road Gwalior-474001(M.P.)
Received on 27 – 09 - 2011 Revised on 20 – 10- 2011 Accepted on 20 – 11 – 20
ABSTRACT
Now days, research on medicinal plants has concerned a lot <strong>of</strong> attention globally. A number <strong>of</strong> confirmations have
been accumulated to express promising potential <strong>of</strong> medicinal plants used in various traditional, complementary and
alternative systems. In recent years a medicinal plant, Calotropis <strong>gigantea</strong> and its major active constituents have
been extensively studied for several <strong>pharmacological</strong> activities. Calotropis <strong>gigantea</strong> (Asclepiadacea) known as Arka
is being used in traditional medicines and contains cardiac glycosides, alkaloids, flavonoids, tannins, reducing
sugars etc. It has been found to have analgesic activity, antipyretic activity, pregnancy interceptive activity, CNS
activity, anti-inflammatory activity, pro-coagulant activity, anti-diarrheal activity, free radical scavenging activity,
antimicrobial activity, anti-tumor activity, antifungal activity, anti-tussive activity, antifeedent activity. To facilitate
the readers to look at their areas <strong>of</strong> interest more easily, the information in the current review have been organised in
various sections according to <strong>pharmacological</strong> <strong>aspects</strong> <strong>of</strong> the plant Calotropis <strong>gigantea</strong> on various health problems.
Key Words: Analgesic, arka, <strong>calotropis</strong> <strong>gigantea</strong>, free radical scavenging activity, traditional medicines.
INTRODUCTION
Calotropis <strong>gigantea</strong> (Asclepiadaceae) is commonly
known as Madar and wild growing tropical plant,
which possesses number <strong>of</strong> medicinal properties.
Humankind first utilized material found in
environment on an empirical basis to cure various
ailments. Natural products from plants and animals
traditionally have provided the pharmaceutical
industry with one <strong>of</strong> its important sources <strong>of</strong> lead
compounds in search <strong>of</strong> new drugs and medicines.
The search for new <strong>pharmacological</strong>ly active agents
from natural resources such as plants, animals and
microbes led to discovery <strong>of</strong> many clinically useful
drugs 1 .
* For Correspondence:
Anurag Agrawal
Department Of Pharmacology
R.C.Patel Institute Of Pharmaceutical Education &
Research
Near Karwand Naka, Shirpur, Dhule (M.S.)-425405
E-Mail: anu2pharma@gmail.com
Mob: +91-9685824456.
It is reported to contain cardiac glycosides, -
sitosterol, madrine, saponins, alkaloids, tannins,
trisecharoides and flavonols. The plant has been used
for various disease condition,including leprosy,
ulcers, tumours and piles. Various <strong>pharmacological</strong>
activity reported like analgesic activity,anti-fertility,
anti-inflammatory activity, hepato-protective activity,
antimyocardial infraction activity and antidirrhreal
activity.
PHARMACOLOGICAL ACTIVITIES
1. Studies on anti-diarrhoeal activity <strong>of</strong>
Calotropis <strong>gigantea</strong> r.br. in experimental
animals. The anti-diarrheal effect <strong>of</strong>
hydroalcoholic (50:50) extract <strong>of</strong> aerial part <strong>of</strong>
Calotropis <strong>gigantea</strong> was studied against castor
oil-induced-diarrhea model in rats. The
gastrointestinal transit rate was expressed as the
percentage <strong>of</strong> the longest distance traversed by
the charcoal divided by the total length <strong>of</strong> the
small intestine. The weight and volume <strong>of</strong>
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intestinal content induced by castor oil were
studied by enteropooling method. 1
2. Studies on proteinases from Calotropis
<strong>gigantea</strong> latex. I. Purification and some
properties <strong>of</strong> two proteinases containing
carbohydrate. Two proteinase containing
carbohydrate, called calotropain-FI and
calotropain-FII, were purified from Calotropis
<strong>gigantea</strong> latex by CM-Sephadex C-50
chromatography. Both calotropain-FI and FII
were found to be homogeneous by rechromatography
on CM-Sephadex C-50, gel
filtration on Sephadex G-100, electrophoresis on
polyacrylamide gel and by N-terminal amino
acid analysis. Some properties <strong>of</strong> these enzymes
are reported. 2
3. Comparative studies on calotropins DI and DII
from the latex <strong>of</strong> Calotropis <strong>gigantea</strong>.
Autodigestion <strong>of</strong> two cysteine proteinases,
calotropins DI and DII isolated from the latex <strong>of</strong>
Calotropis <strong>gigantea</strong>, has been studied at pH 7.5 and
37 degrees C in the presence <strong>of</strong> an activating agent.
Calotropin DI is more susceptible to autodigestion
than calotropin DII. During autodigestion no
interconversion <strong>of</strong> one calotropin to another has
occurred, as verified by polyacrylamide gel
electrophoresis in the presence and absence <strong>of</strong>
sodium dodecyl sulfate. Immunologically, both
calotropins are closely related, but they differ from
papain and ficin. Both calotropins block N-terminal
amino acid residues. 3
4. Studies on proteinases from Calotropis
<strong>gigantea</strong> latex. II. Physico-chemichal
properties <strong>of</strong> calotropain-FI and FII. The
molecular weights <strong>of</strong> purified calotropain-FI and
FII were determined by sodium dodecyl
sulphate-polyacrylamide gel electrophoresis and
by filtration <strong>of</strong> Sephadex G-100. Activation <strong>of</strong>
calotropain-FI and FII by different sulfhydryl
activators was studied. The results obtained from
inhibition studies by various enzyme-modifying
reagents suggest the possible role <strong>of</strong> cysteine and
histidine residues in the active site <strong>of</strong> both the
enzymes. The free and total sulfhydryl contents
<strong>of</strong> both the enzymes were determined by the use
<strong>of</strong> 5-5'-dithio-bis-2-nitrobenzoic acid. Total
amino acid compositions <strong>of</strong> both the enzymes
were also determined. A comparative study <strong>of</strong>
the esterase, amidase, milk-clotting and
caseinolytic activities <strong>of</strong> calotropain-FI and FII
are also presented. 4
5. Evaluation <strong>of</strong> antipyretic activity <strong>of</strong> Calotropis
<strong>gigantea</strong> (Asclepiadaceae) in experimental
animals. The roots <strong>of</strong> Calotropis <strong>gigantea</strong> have
been used in leprosy, eczema, syphilis,
elephantiasis, ulceration and cough in the Indian
system <strong>of</strong> traditional medicine. The present
review reveals its antipyretic activity by using
yeast-induced and TAB (Typhoid) vaccineinduced
pyrexia in rats and rabbits. In both yeastinduced
and TAB vaccine-induced fever, the
fever was significantly reduced and the body
temperature was normalized by administration <strong>of</strong>
200 and 400 mg/kg dose <strong>of</strong> Calotropis <strong>gigantea</strong>
extract intraperitoneally. Based on the results <strong>of</strong>
the present study it can be concluded that the
extract <strong>of</strong> C.<strong>gigantea</strong> has potential antipyretic
activity against both yeast-induced and TAB
vaccine-induced fever, indicating the possibility
<strong>of</strong> developing C.<strong>gigantea</strong> as a cheaper and potent
antipyretic agent. 5
6. Procoagulant activity <strong>of</strong> Calotropis <strong>gigantea</strong>
latex associated with fibrin(ogen)olytic
activity. The crude latex extract contained many
proteins, which are highly basic in nature and
exhibited strong proteolytic activity. The crude
extract hydrolyses casein, human fibrinogen and
crude fibrin clot in a dose-dependent manner.
The hydrolyzing activity was completely
inhibited by IAA indicating that they belong to
the super family, cysteine proteases. Crude
extract hydrolyses Alpha, Beta and gamma
subunits <strong>of</strong> fibrinogen. Among all the subunits
the preferential subunit to get hydrolyzed was
Alpha followed by Beta and gamma subunit is
highly resistant and hydrolyzed at higher protein
concentration or over a prolonged incubation
time. The crude extract hydrolysis crude fibrin
clot strongly compared to trypsin and papain.
Pharmacologically the crude extract is
hemorrhagic and induces skin hemorrhage at >75
microgram and reduces coagulation time <strong>of</strong>
citrated plasma from 150 to 47 s and promotes
blood coagulation. 6
7. Pregnancy interceptive activity <strong>of</strong> the roots <strong>of</strong>
Calotropis <strong>gigantea</strong> Linn. in rats. The ethanolic
extract <strong>of</strong> the roots <strong>of</strong> C.<strong>gigantea</strong> Linn. exhibited
100% pregnancy interceptive activity in rats
when administered as a single oral dose <strong>of</strong> 100
mg/kg on Day 1 postcoitum. The extract also
exhibited 100% efficacy at the dose <strong>of</strong> 12.5
mg/kg when administered in the Days 1-5 and 1-
7 postcoitum schedules. When C.<strong>gigantea</strong> Linn.
was administered during the peri-cum-early post
implantation period (i.e., Days 5-7 postcoitum at
250 mg/kg), most <strong>of</strong> the implantations showed
signs <strong>of</strong> resorption. On fractionation, the
chlor<strong>of</strong>orm fraction showed 100% activity at 100
mg/kg in the single-day (Day 1 postcoitum)
schedule, whereas the hexane, n-butanol-soluble
and n-butanol-insoluble fractions were found to
be inactive at this dose. At autopsy on Day 10
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postcoitum, 7-25% loss in body weight was
recorded at the minimum effective contraceptive
dose (MED) in rats treated with the ethanolic
extract as well as its chlor<strong>of</strong>orm-soluble fraction
on Days 1-7, 1-5 and 1 postcoitum, in
comparison with the 6-7% increase in body
weight observed in vehicle control rats. There
was however no mortality in any <strong>of</strong> the treatment
groups. The active ethanolic extract and its
chlor<strong>of</strong>orm fraction were devoid <strong>of</strong> any estrogen
agonistic or antagonistic activity at their
respective MEDs in the ovariectomized
immature rat bioassay. 7
8. Phytoremediation <strong>of</strong> radiostrontium 90 (Sr)
and radiocesium 137 (Cs) using giant milky
weed (Calotropis <strong>gigantea</strong> R.Br.) plants.
Potential <strong>of</strong> plants to remove radio nuclides/toxic
elements from soils and solutions can be
successfully applied for removal <strong>of</strong> important
radio nuclides such as strontium-90 ((90)Sr) and
cesium-137 ((137)Cs). When uptake <strong>of</strong> (137)Cs
and (90)Sr by Calotropis <strong>gigantea</strong> plants
incubated in distilled water spiked with the
radionuclides either alone or in combination was
studied, it was found to have a high efficiency
for the removal <strong>of</strong> (90) Sr, with 90% being
removed from solutions (5x10(3)kBql(-1))
within 24h <strong>of</strong> incubation. However, in case <strong>of</strong>
(137) Cs, about 44% could be removed from
solutions (5x10(3)kBql(-1)) at the end <strong>of</strong> 168h <strong>of</strong>
incubation. Accumulation <strong>of</strong> (90)Sr and (137)Cs
was higher in roots compared to shoots. The
plants could remediate both (90)Sr and (137)Cs
when they were added together to the solution.
When two months old plants were incubated in
low level nuclear waste, 99% <strong>of</strong> activity
disappeared at the end <strong>of</strong> 15 days. The present
study suggests that C. <strong>gigantea</strong> could be used as
a potential candidate plant for phytoremediation
<strong>of</strong> (90)Sr and (137)Cs. 8
9. Flavonol glycosides from Calotropis <strong>gigantea</strong>.
Besides isolation and characterization <strong>of</strong>
isorhamnetin-3-O-rutinoside, isorhamnetin-3-Oglucopyranoside
and taraxasteryl acetate, a new
flavonol trisaccharide was isolated from the
aerial parts <strong>of</strong> Calotropis <strong>gigantea</strong>, and its
structure was established as isorhamnetin-3-O-
[2-O-beta-D-galactopyranosyl-6-O-alpha-Lrhamnopy
ranosyl]- beta-D-glucopyranoside by a
combination <strong>of</strong> fast atom bombardment mass
spectroscopy, 1H and 13C NMR spectra and
some chemical degradations. 9
10. Indonesian medicinal plants. I. Chemical
structures <strong>of</strong> calotroposides A and B, two new
oxypregnane-oligoglycosides from the root <strong>of</strong>
Calotropis <strong>gigantea</strong> (Asclepiadaceae). Two new
oxypregnane-oligoglycosides
named
calotroposides A (1) and B (2) have been
isolated from the root <strong>of</strong> Calotropis <strong>gigantea</strong>
(Asclepiadaceae), an Indonesian medicinal plant,
and their chemical structures have been
elucidated by chemical and spectroscopic
methods as 12-O-benzoyllineolon 3-O-beta-Dcymaropyranosyl(1----4)-beta-Doleandropyranosyl(
1----4)- beta-Doleandropyranosyl(1----4)-beta-Dcymaropyranosyl(1----4)-beta-Dcymaropyranoside
and 12-Obenzoyldeacetylmetaplexigenin
3-O-beta-Dcymaropyranosyl(1---4)-beta-Doleandropyranosyl(-
---4)- beta-Doleandropyranosyl(1----4)-beta-Dcymaropyranosyl(1---
-4)- beta-Dcymaropyranoside,
respectively. 10
11. A Novel Insect Antifeedant Nonprotein
Amino Acid from Calotropis <strong>gigantea</strong>:
Giganticine (1), a novel nonprotein amino acid,
has been isolated from a methanol extract <strong>of</strong> the
root bark <strong>of</strong> Calotropis <strong>gigantea</strong> and its structure
established by spectroscopic methods. It
exhibited a significant antifeedant activity
against nymphs <strong>of</strong> the desert locust Schistocerca
gregaria. 11
12. Cytotoxic principles <strong>of</strong> a Bangladeshi crude
drug, akond mul (roots <strong>of</strong> Calotropis <strong>gigantea</strong>
L.). Three cardenolide glycosides, calotropin (1),
frugoside (2), and 4'-O-beta-Dglucopyranosylfrugoside
(3), were obtained as
the cytotoxic principles <strong>of</strong> "akond mul" (roots <strong>of</strong>
Calotropis <strong>gigantea</strong> L.). The cytotoxicity <strong>of</strong>
these compounds against various cell lines <strong>of</strong>
human and mouse origin was tested. They
showed similar cell line selectivity to those <strong>of</strong>
cardiac glycosides such as digoxin and ouabain:
they are toxic to cell lines <strong>of</strong> human origin, but
not to those derived from mouse origin at 2 µ/ml.
12
13. CNS activity <strong>of</strong> Calotropis <strong>gigantea</strong> roots.
Alcoholic extract <strong>of</strong> peeled roots <strong>of</strong> Calotropis
<strong>gigantea</strong>n (Asclepiadaceae) was tested orally in
albino rats at the dose level <strong>of</strong> 250 and 500mg/kg
bodyweight for CNS activity. Prominent
analgesic activity was observed in Eddy's hot
plate method and acetic acid induced writhing.
The paw licking time was delayed and the
numbers <strong>of</strong> writhings were greatly reduced.
Significant anticonvulsant activity was seen as
there was a delay in the onset <strong>of</strong>
pentylenetetrazole induced convulsions as well
as decrease in its severity. The extract treated
rats spent more time in the open arm <strong>of</strong> EPM
showing its antianxiety activity. There was a
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decrease in the locomotor activity. The fall <strong>of</strong>f
time (motor coordination) was also decreased. A
potentiation in the pentobarbitone-induced sleep
due to the sedative effect <strong>of</strong> the extract was
observed. No mortality was seen upto the dose <strong>of</strong>
1g/kg. These results show the analgesic,
anticonvulsant, anxiolytic and sedative effect <strong>of</strong>
the extract. 13
14. 19-Nor- and 18, 20-Epoxy-cardenolides from
the Leaves <strong>of</strong> Calotropis <strong>gigantea</strong>. Two new
cardenolides (1 and 2) along with 12 known
compounds were isolated from the
dichloromethane extract <strong>of</strong> the leaves <strong>of</strong>
Calotropis <strong>gigantea</strong>. The structural elucidation
was accomplished by spectroscopic methods.
Some <strong>of</strong> the isolates were evaluated for cytotoxic
activity against KB, BC, and NCI-H187 cancer
cell lines, and all cardenolides tested were found
to possess strong inhibitory effects. The presence
<strong>of</strong> a deoxysugar at C-3, a formyl group at C-10,
and an alpha,beta-unsaturated gamma-lactone
was crucial for cytotoxic activity. 14
15. Analgesic activity <strong>of</strong> Calotropis <strong>gigantea</strong>
flower. The alcoholic extract <strong>of</strong> the flowers <strong>of</strong>
Calotropis <strong>gigantea</strong> was administered orally and
explored for its analgesic activity in chemical
and thermal models in mice. In acetic acid
induced writhing test, an inhibition <strong>of</strong> 20.97%
and 43.0% in the number <strong>of</strong> writhes was
observed at the doses <strong>of</strong> 250 and 500 mg/kg,
respectively. In the hot plate method the paw
licking time was delayed. The analgesic effect
was observed after 30 min <strong>of</strong> dose administration
which reached its maximum after 90 min. 15
16. Evaluation <strong>of</strong> anti-inflammatory activity <strong>of</strong>
Calotropis <strong>gigantea</strong> in various biological
systems. The anti-inflammatory activity was
evaluated using carrageenin-induced, kaolin -
induced rat paw oedema for acute inflammation
and cotton-pellet granuloma, adjuvant-induced
arthritis model for chronic inflammation.
Antipyretic activity was carried out using yeast
induced pyresis method. Phenylquinone--
induced writhing method in mice was also used
for evaluation <strong>of</strong> analgesic activity. Test
compounds exhibited variable anti-inflammatory
activity and peak activity <strong>of</strong> the test compounds
were reached at 2 h. Alkaloid fraction possesses
comparatively high initial anti-inflammatory
activity. The residual anti-inflammatory activity
<strong>of</strong> alkaloid fraction <strong>of</strong> Calotropis <strong>gigantea</strong>
suggest either a greater protein binding nature <strong>of</strong>
the compound there by providing a slow released
pool <strong>of</strong> active drug molecule in the system or
non available <strong>of</strong> possible bioactive metabolites to
retain the activity pr<strong>of</strong>ile relation. Evaluation <strong>of</strong>
the effect <strong>of</strong> Calotropis gingantea in various
experimental animal models. The antiinflammatory
activity was evaluated using
carrageenin-induced, kaolin-induced rat paw
oedema for acute and cotton-pellet granuloma,
adjuvant-induced arthritis model for chronic
inflammation. Antipyretic activity was carried
out using yeast induced pyresis method. 16
17. Heavy metal and nutrient concentration in
soil and plants growing on a metalliferous
chromite minespoil: Metal contamination in
soil and plant samples from a chromite mine and
its adjoining regions was determined. The metal
concentration varied in stem, leaf and root <strong>of</strong>
different tree species. In the case <strong>of</strong> shrubs, the
highest concentration <strong>of</strong> iron (18.5 mg kg(-1)
was detected in the stem <strong>of</strong> Combretum
roxburghii. The concentration <strong>of</strong> aluminium
varied from 1.8 - 5.3 mg kg(-1) dry weight,
whereas the nickel content was found to be the
highest in the stem <strong>of</strong> Calotropis <strong>gigantea</strong>. In the
case <strong>of</strong> herbs, chromium concentration was
highest (60.9 mg kg(-1) dry weight) in Evovulus
alsenoides and the lowest (18.8 mg kg(-1) dry
weight) in Andrographis paniculata. There was a
significant correlation observed between
chromium in soil with the root <strong>of</strong> tree species
like Lagerstroemia parviflora, Madhuca
longifolia, Anogeissus latifolia and Haldina
cordyfolia. Nickel in soil was significantly
correlated with the stem and leaf <strong>of</strong> all the tree
species except Chlroxylon sweitenta. Iron in soil
showed correlation with the stem and leaf <strong>of</strong>
Chloroxylon sweitenia. Among the shrubs
(Calotropis <strong>gigantea</strong>, Combretum roxburghii
and Smilax zeylancia), chromium in soil showed
a correlation with the root. Nickel in soil was
positively correlated with the stem and leaf <strong>of</strong>
Calotropis <strong>gigantea</strong> and Combretum roxburghii.
Among the herbs, chromium in the whole plant
<strong>of</strong> Evolvulus alsenoids, Solanum surattense and
Phyllanthus fraternus showed significant positive
correlation with soil; nickel in Solanum
surattense showed significant positive correlation
with soil. The positive correlation coefficient
was observed between iron in the whole plant
and soil on Phyllanthus virgatus, Phyllanthus
fraternus and Andrographis paniculata. The
above information would be useful for the
establishment <strong>of</strong> a vegetation cover on the mine
waste heaps. 17
18. Comparative Study on Plant Latex Proteases
and their Involvement in Hemostasis: A
Special Emphasis on Clot Inducing and
Dissolving Properties. In the present study we
compared the clot inducing and dissolving
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properties <strong>of</strong> Calotropis <strong>gigantea</strong> R. Br.
(Asclepiadaceae), Synadenium grant Hook. f.
(Euphorbiaceae) and Wrightia Tinctoria R. Br.
(Apocynaceae) latex extracts. Both
fibrinogenolytic and fibrinolytic activity potency
<strong>of</strong> the extracts were in the order <strong>of</strong> C. <strong>gigantea</strong> >
S. grantii > W. tinctoria. Among the three
latices, C. <strong>gigantea</strong> is toxic with a minimum
hemorrhagic dose (MHD) <strong>of</strong> > 75 mug, whereas
S. grantii and W. tinctoria latex extracts were
non-toxic and did not induce any hemorrhagic
effect at the tested dose (> 200 mug). 18
19. Development-inhibiting activity <strong>of</strong> some
tropical plants against Sitophilus zeamais
Motschulsky (Coleoptera: Curculionidae).
Thirteen tropical plants were evaluated for
development-inhibiting activity against
Sitophilus zeamais. The bioassays were carried
out by incorporating seeds or leaves at various
dose levels into an artificial diet for the test
insect. It was found that seeds <strong>of</strong> Basella alba
and leaves <strong>of</strong> Operculina turpethum and
Calotropis <strong>gigantea</strong> were potent in delaying
development and in reducing adult emergence,
and hence the capacity for population increase.
At 0.5% concentration, adult emergence in tests
with B. alba, O. turpethum and Calotropis
<strong>gigantea</strong> was reduced by 62, 95 and 70%,
respectively. In B. alba and Calotropis <strong>gigantea</strong>,
the development periods were 2.2 and 1.8 times
those in the control and the capacities for
increase/day were only 0.0324 and 0.0328
compared with 0.1004 in the control. B. alba, O.
turpethum and Calotropis <strong>gigantea</strong> were active
at concentrations as low as 0.01, 0.05 and 0.1%.
The potential <strong>of</strong> these materials in insect pest
management is discussed. 19
20. Influence <strong>of</strong> host plant on growth and
reproduction <strong>of</strong> Aphis nerii and feeding and
prey utilization <strong>of</strong> its predator Menochilus
sexmaculatus. Influence <strong>of</strong> different
physiological stages (young, mature and
senescent) <strong>of</strong> Calotropis <strong>gigantea</strong> leaves on
growth and reproductive ability <strong>of</strong> A. nerii and
feeding, prey utilization, fecundity and lipid
content <strong>of</strong> its predator M. sexmaculatus were
investigated. Increased reproductive period, total
life span and reproduction <strong>of</strong> nymphs per female
<strong>of</strong> A. nerii were observed when reared on mature
leaves. This relative preference <strong>of</strong> A. nerii and
maximum utilization <strong>of</strong> mature leaves as
compared to other physiological aged leaves are
mainly due to changes in the chemical
composition such as protein, carbohydrate, lipid,
amino acid, nitrogen and phenolic <strong>of</strong> Calotropis
<strong>gigantea</strong>. Further, aphids reared on mature
leaves influenced its predator's (M.
sexmaculatus) growth, prey utilization and
reproductive performances. Fecundity and
longevity were high, while developmental time
<strong>of</strong> predator was shorter on mature leaves fed
aphid. Maximum prey utilization and increased
efficiency <strong>of</strong> ingested and digested food <strong>of</strong>
predator was observed on mature leaves reared
aphid. The results are interpreted and discussed
in relation to plant aphid and predator interaction
(tritrophic). 20
21. Mitochondrial malate dehydrogenase and
malic enzyme <strong>of</strong> a filarial worm Setaria
digitata: some properties and effects <strong>of</strong> drugs
and herbal extracts. Mitochondrial malate
dehydrogenase (mMDH) and malic enzyme
(mME) <strong>of</strong> a filarial worm Setaria digitata were
studied. mMDH exhibited the highest activities
in the oxidation and reduction reactions at pH
9.5 and pH 6.2, respectively, while mME did so
in the malate decarboxylation reaction at pH 6.8.
mME showed no detectable activity on the
pyruvate carboxylation direction. The Km values
for malate (1.7 mM) and oxaloacetate (0.17 mM)
and the ratio <strong>of</strong> Vmax oxidation: Vmax
reduction (2.73) tend to favor the oxaloacetate
reduction by mMDH. mME showed a relatively
high Km value <strong>of</strong> 8.3 mM, for malate
decarboxylation. A drug, diethylcarbamazine
citrate (DEC-C), did not change appreciably the
activity <strong>of</strong> either mMDH or mME, while filarin
(a drug <strong>of</strong> herbal origin) effectively inhibited
mMDH. The leaf extracts <strong>of</strong> Ocimum sanctum,
Lawsonia inermis and Calotropis <strong>gigantea</strong> and
leaf and flower extracts <strong>of</strong> Azadirachta indica
were, however, found to inhibit both mMDH and
mME. 21
22. Crystal and molecular structure <strong>of</strong> the
sulfhydryl protease calotropin DI at 3.2 A
resolution. The three-dimensional structure <strong>of</strong>
the sulfhydryl protease calotropin DI isolated
from the madar plant i.e. Calotropis <strong>gigantea</strong>,
has been determined at 3.2, a resolution using the
multiple isomorphous replacement method with
five heavy atom derivatives. A Fourier synthesis
based on protein phases with a mean figure <strong>of</strong>
merit <strong>of</strong> 0.857 was used for model building. The
polypeptide backbone <strong>of</strong> calotropin DI is folded
to form two distinct lobes, one <strong>of</strong> which is
comprised mainly <strong>of</strong> alpha-helices, while the
other is characterized by a system <strong>of</strong> all
antiparallel pleated sheets. The overall molecular
architecture closely resembles those found in the
sulfhydryl proteases papain and actinidin.
Despite the unknown amino acid sequence <strong>of</strong>
calotropin DI a number <strong>of</strong> residues around its
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active center could be identified. These amino
acid side-chains were found in a similar
arrangement as the corresponding ones in papain
and actinidin. The polypeptide chain between
residues 1 and 18 <strong>of</strong> calotropin DI folds in a
unique manner, providing a possible explanation
for the unusual inability <strong>of</strong> calotropin DI to
hydrolyze those synthetic substrates on which
papain and actinidin act upon. 22
23. Chemical study <strong>of</strong> Indonesian medicinal
plants. A series <strong>of</strong> scientific expeditions in
Indonesia for collecting informations and
materials concerning locally used medicinal
plants and Javanese traditional medicine "jamu"
have been carried out by us since 1985. This
pharmacochemical investigations <strong>of</strong> nine
Indonesian medicinal plants: i.e. Pongamia
pinnata (Papilionaceae), Fagara rhetza
(Rutaceae), Calotropis <strong>gigantea</strong>
(Asclepiadaceae), Beilschmiedia madang
(Lauraceae), Caesalpinia major (Fabaceae),
Peronema canescens (Verbenaceae), Taxus
sumatrana (Taxaceae), Alyxia reinwardtii
(Apocynaceae), and Merremia mammosa
(Convolvulaceae), which were selected among
plant materials collected in those surveys. 23
24. Effect <strong>of</strong> plant extracts and systemic fungicide
on the pineapple fruit-rotting fungus,
Ceratocystis paradoxa: Antifungal activities <strong>of</strong>
extracts <strong>of</strong> sixteen plants were tested against
Ceratocystis paradoxa which causes s<strong>of</strong>t rot <strong>of</strong>
pineapples. Xanthium strumarium was the most
effective followed by Allium sativum. The
effectiveness <strong>of</strong> various extracts against C.
paradoxa was in the decreasing order <strong>of</strong>
Meriandra bengalensis, Mentha piperita,
Curcuma longa, Phlogacanthus thyrsiflorus,
Toona ciliata, Vitex negundo, Azadirachta
indica, Eupatorium birmanicum, Ocimum
sanctum and Leucas aspera. Extracts <strong>of</strong> Cassia
tora, Gynura cusimba, Calotropis <strong>gigantea</strong> and
Ocimum canum showed poor fungitoxicity.
Ethanol was suitable for extraction <strong>of</strong> the
inhibitory substance from X. strumarium.
Acetonitrile was highly toxic to this fungus.
Millipore filter-sterilized extracts had a more
inhibitory effect on the fungus than the
autoclaved samples. Treatment <strong>of</strong> pineapple
fruits infested with C. paradoxa by X.
strumarium extract reduced the severity <strong>of</strong> the
disease. 24
25. Asaia siamensis sp. nov., an acetic acid
bacterium in the alpha-proteobacteria. Five
bacterial strains were isolated from tropical
flowers collected in Thailand and Indonesia by
the enrichment culture approach for acetic acid
bacteria. Phylogenetic analysis based on 16S
rRNA gene sequences showed that the isolates
were located within the cluster <strong>of</strong> the genus
Asaia. The isolates constituted a group separate
from Asaia bogorensis on the basis <strong>of</strong> DNA
relatedness values. Their DNA G+C contents
were 58.6-59.7 mol%, with a range <strong>of</strong> 1.1 mol%,
which were slightly lower than that <strong>of</strong> A.
bogorensis (59.3-61.0 mol%), the type species <strong>of</strong>
the genus Asaia. The isolates had morphological,
physiological and biochemical characteristics
similar to A. bogorensis strains, but the isolates
did not produce acid from dulcitol. On the basis
<strong>of</strong> the results obtained, the name Asaia siamensis
sp. nov. is proposed for these isolates. Strain
S60-1T, isolated from a flower <strong>of</strong> crown flower
(dok rak, Calotropis <strong>gigantea</strong>) collected in
Bangkok, Thailand, was designated the type
strain (= NRIC 0323T = JCM 10715T = IFO
16457T). 25
26. Evaluation <strong>of</strong> chemical constituents and freeradical
scavenging activity <strong>of</strong> Swarnabhasma
(gold ash), an ayurvedic drug: Swarnabhasma
was prepared after proper purification and
calcination as per Ayurvedic pharmacy which
consisted <strong>of</strong> Realger (As(2)S(2)), Lead oxide
(Pb(3)O(4)), Pure gold (Au) and Latex <strong>of</strong>
Calotropis <strong>gigantea</strong>. Qualitative analyses
indicated that Swarnabhasma contained not only
gold but also several microelements (Fe, Al, Cu,
Zn, Co, Mg, Ca, As, Pb, etc.). The metal content
in the bhasma was determined by atomic
absorption spectrometry. Acute oral
administration <strong>of</strong> Swarnabhasma showed no
mortality in mice (up to 1 ml /20 g b.w. <strong>of</strong>
Swarnabhasma suspension containing 1mg <strong>of</strong>
drug). Chronic administration <strong>of</strong> Swarnabhasma
also showed no toxicity as judged by SGPT,
SGOT, serum creatinine and serum urea level
and histological studies. In an experimental
animal model, chronic Swarnabhasma-treated
animals showed significantly increased
superoxide dismutase and catalase activity, two
enzymes that reduce free radical concentrations
in the body. The ethanolic extracts <strong>of</strong> leaf and
latex <strong>of</strong> Calotropis procera and Calotropis
gingantea (Asciepadiacea) were tested for free
radical Scavenging activity using 1,1 Dipthenyl
Picryl hydrazyl radicas. The latex extracts <strong>of</strong> C.
procera and C. gigeantea (10 mg/ml) exhibited
greater capacity to scavenge DPPH radicals
whereas leaf extract showed moderate free
radical scavenging activity. 26
27. Hepatoprotactive activity
Alcoholic extract <strong>of</strong> C.<strong>gigantea</strong> leaf reveals good
hepatoprotective activity in dose dependent
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Anurag Agrawal., et al. / International Journal <strong>of</strong> Advances in Pharmaceutical Research
manner against CCl 4 induced hepatotoxicity in
rats. 27 Leaf extract showed antitussive activity
due to presence <strong>of</strong> alkaloids and glycosides.
CONCLUSION
Present article highlights the recent researches on
Calotropis <strong>gigantea</strong>. It is a well known herbal
drug used to treat various diversified
physiological conditions. The plant Calotropis
<strong>gigantea</strong> has a wide array <strong>of</strong> <strong>pharmacological</strong>
activities and many isolated compounds <strong>of</strong> the
plant lack study on their <strong>pharmacological</strong>
activities. Therefore it is worthwhile validating
the <strong>pharmacological</strong> properties <strong>of</strong> Calotropis
<strong>gigantea</strong>, which will substantiate the use <strong>of</strong> this
plant over countries for medicinal purposes.
Calotropis <strong>gigantea</strong> imbibing a tremendous
potential, deserves a special attention <strong>of</strong> the
scientific fraternity. The results encountered in
various investigations reveal important
<strong>pharmacological</strong> activities <strong>of</strong> the plants which
may be used as leads in developing novel
therapeutic agents.
In recent years, ethno-botanical and traditional
uses <strong>of</strong> natural compounds, especially those <strong>of</strong>
plant origin, have received much attention as
they are well known for their efficacy and are
generally believed to be safe for human use. It is
best to use the classical approach in the search
for new molecules to manage a variety <strong>of</strong>
diseases. A thorough review <strong>of</strong> the published
literature on Calotropis <strong>gigantea</strong> shows that it is
a popular remedy in a variety <strong>of</strong> ethnic groups,
as well as Ayurvedic and traditional practitioners
for the treatment <strong>of</strong> a range <strong>of</strong> ailments.
Researchers are exploring the therapeutic
potential <strong>of</strong> this plant as it is likely to have more
therapeutic properties than are currently known.
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